Pronunciation:

boe-SUE-ti-nib

Brand Names:

• Bosulif

Dosage Forms:

• Capsule
• Tablet

Classifications:

Therapeutic—

Antineoplastic Agent

Pharmacologic—

Tyrosine Kinase Inhibitor

Uses of This Medicine:

Bosutinib is used to treat chronic phase (CP) Philadelphia chromosome-positive chronic myelogenous leukemia (Ph+ CML) in patients who are newly-diagnosed or who have taken other medicines that did not work well. This medicine is also used to treat accelerated phase (AP) or blast phase (BP) Ph+ CML in patients who have taken other medicines but did not work well. Leukemia is a type of cancer where the body makes abnormal white blood cells.

Bosutinib is an antineoplastic (cancer) medicine. It interferes with the growth of cancer cells, which are eventually destroyed by the body. Since the growth of normal cells may also be affected by bosutinib, other side effects can occur. Before you begin treatment, talk to your doctor about the benefits of this medicine as well as the possible risks of using it.

This medicine is available only with your doctor's prescription.

Before Using This Medicine:

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies—

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Children—

Appropriate studies have not been performed on the relationship of age to the effects of bosutinib to treat CP Ph+ CML in children younger than 1 year of age and to treat AP Ph+ CML or BP Ph+ CML in children. Safety and efficacy have not been established.

Older adults—

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of bosutinib in the elderly.

Breast-feeding—

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Other medicines—

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

• Levoketoconazole
• Measles Virus Vaccine, Live
• Mumps Virus Vaccine, Live
• Rotavirus Vaccine, Live
• Rubella Virus Vaccine, Live
• Varicella Virus Vaccine, Live
• Zoster Vaccine, Live

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Adagrasib
• Adenovirus Vaccine, Live
• Amprenavir
• Aprepitant
• Asciminib
• Atazanavir
• Avacopan
• Bacillus of Calmette and Guerin Vaccine, Live
• Belzutifan
• Berotralstat
• Boceprevir
• Carbamazepine
• Ceritinib
• Cholera Vaccine, Live
• Cimetidine
• Ciprofloxacin
• Clarithromycin
• Clofazimine
• Cobicistat
• Conivaptan
• Crizotinib
• Cyclosporine
• Dabrafenib
• Daridorexant
• Darunavir
• Dengue Tetravalent Vaccine, Live
• Dexlansoprazole
• Diltiazem
• Dronedarone
• Duvelisib
• Ebola Zaire Vaccine, Live
• Enasidenib
• Enzalutamide
• Erythromycin
• Esomeprazole
• Fedratinib
• Fexinidazole
• Fluconazole
• Fluvoxamine
• Fosamprenavir
• Fosnetupitant
• Fosphenytoin
• Idelalisib
• Imatinib
• Indinavir
• Influenza Virus Vaccine, Live
• Itraconazole
• Ivosidenib
• Ketoconazole
• Lanreotide
• Lansoprazole
• Larotrectinib
• Lefamulin
• Lenacapavir
• Letermovir
• Lonafarnib
• Lorlatinib
• Lumacaftor
• Mavacamten
• Mifepristone
• Mitapivat
• Mitotane
• Mobocertinib
• Nefazodone
• Nelfinavir
• Netupitant
• Nilotinib
• Nirogacestat
• Octreotide
• Olutasidenib
• Omaveloxolone
• Omeprazole
• Pacritinib
• Palbociclib
• Pantoprazole
• Phenobarbital
• Phenytoin
• Pirtobrutinib
• Poliovirus Vaccine, Live
• Posaconazole
• Primidone
• Rabeprazole
• Repotrectinib
• Ribociclib
• Rifampin
• Rifapentine
• Ritlecitinib
• Ritonavir
• Saquinavir
• Schisandra sphenanthera
• Selpercatinib
• Smallpox Monkeypox Vaccine, Live Non-Replicating
• Smallpox Vaccine
• Sotorasib
• St John's Wort
• Taurursodiol
• Telaprevir
• Telithromycin
• Tocilizumab
• Trofinetide
• Troleandomycin
• Tucatinib
• Typhoid Vaccine, Live
• Verapamil
• Vonoprazan
• Voriconazole
• Voxelotor
• Yellow Fever Vaccine

Other interactions—

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

• Grapefruit Juice

Other medical problems—

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Anemia (low red blood cells) or
• Blood or bone marrow problems or
• Diabetes, history of or
• Edema (fluid retention or swelling) or
• Heart or blood vessel disease or
• Heart failure, or history of or
• Hypertension (high blood pressure) or
• Neutropenia (low white blood cells) or
• Thrombocytopenia (low platelets in the blood)—Use with caution. May make these conditions worse.

• Infection—May decrease your body's ability to fight infection.

• Kidney disease or
• Liver disease—Use with caution. The effects may be increased because of slower removal of the medicine from the body.

Proper Use of This Medicine:

Take this medicine exactly as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. To do so may increase the chance of side effects.

This medicine comes with a patient information insert and patient instructions. Read and follow the instructions carefully. Ask your doctor if you have any questions.

You may take this medicine with food.

Swallow the tablet whole. Do not cut, crush, break, or chew it.

Swallow the capsule whole. If you are unable to swallow the capsule whole:

• Gather the supplies (eg, container, applesauce or yogurt, teaspoon, disposable gloves) needed to prepare the mixture.
• Put on disposable gloves. Add the amount of room temperature applesauce or yogurt needed to the container. Do not use any other food.
• Carefully open the capsule and mix the entire contents with applesauce or yogurt.
• Swallow the mixture right away without chewing. Do not store the mixture for later use.
• Throw away the empty capsule shell in the household thrash.
• Wash the teaspoon and container with soap and warm water. Remove the gloves and throw them away in the household thrash. Wash and dry your hands.

If you are taking an antacid (eg, aluminum hydroxide, magnesium hydroxide, Maalox®, Rolaids®, or Tums®) or stomach medicine, take it at least 2 hours before or after you take bosutinib.

Do not drink grapefruit juice while you are using this medicine. Grapefruit juice may change the amount of medicine that is absorbed in the body.

Dosing—

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For oral dosage form (capsules or tablets):
  • For the treatment of newly-diagnosed CP Ph+ CML:
    • Adults—400 milligrams (mg) once a day. Your doctor may adjust your dose as needed and tolerated. However, the dose is usually not more than 600 mg per day.
    • Children 1 year of age and older—Dose is based on body surface area (BSA) and must be determined by your doctor. Your doctor may adjust your dose as needed and tolerated. However, the dose is usually not more than 600 mg per day.
      • BSA 1.1 meter squared (m2) or greater—400 mg once a day.
      • BSA 0.9 to less than 1.1 m2—300 mg once a day.
      • BSA 0.75 to less than 0.9 m2—250 mg once a day.
      • BSA 0.55 to less than 0.75 m2—200 mg once a day.
      • BSA less than 0.55 m2—150 mg once a day.
    • Children younger than 1 year of age—Use and dose must be determined by your doctor.
  • For the treatment of CP Ph+ CML in patients who have used other treatments that did not work well:
    • Adults—500 milligrams (mg) once a day. Your doctor may adjust your dose as needed and tolerated. However, the dose is usually not more than 600 mg per day.
    • Children 1 year of age and older—Dose is based on body surface area (BSA) and must be determined by your doctor. Your doctor may adjust your dose as needed and tolerated. However, the dose is usually not more than 600 mg per day.
      • BSA 1.1 meter squared (m2) or greater—500 mg once a day.
      • BSA 0.9 to less than 1.1 m2—400 mg once a day.
      • BSA 0.75 to less than 0.9 m2—350 mg once a day.
      • BSA 0.63 to less than 0.75 m2—300 mg once a day.
      • BSA 0.55 to less than 0.63 m2—250 mg once a day.
      • BSA less than 0.55 m2—200 mg once a day.
    • Children younger than 1 year of age—Use and dose must be determined by your doctor.
  • For the treatment of AP Ph+ CML or BP Ph+ CML in patients who have used other treatments that did not work well:
    • Adults—500 milligrams (mg) once a day. Your doctor may adjust your dose as needed and tolerated. However, the dose is usually not more than 600 mg per day.
    • Children—Use and dose must be determined by your doctor.

Missed dose—

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

If you miss a dose of this medicine and it has been more than 12 hours, skip the missed dose and go back to your regular dosing schedule.

Storage—

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Precautions While Using This Medicine:

It is very important that your doctor check your progress at regular visits to make sure that this medicine is working properly. Blood and urine tests may be needed to check for unwanted effects.

Using this medicine while you are pregnant can harm your unborn baby. If you are a woman who can get pregnant, your doctor may do tests to make sure you are not pregnant. Use an effective form of birth control to keep from getting pregnant during treatment with this medicine and for at least 2 weeks after the last dose. If you think you have become pregnant while using this medicine, tell your doctor right away.

Bosutinib can temporarily lower the number of white blood cells in your blood, increasing the chance of getting an infection. It can also lower the number of platelets, which are necessary for proper blood clotting. If this occurs, there are certain precautions you can take, especially when your blood count is low, to reduce the risk of infection or bleeding:

• If you can, avoid people with infections. Check with your doctor right away if you think you are getting an infection or if you get a fever or chills, cough or hoarseness, lower back or side pain, or painful or difficult urination.
• Check with your doctor right away if you notice any unusual bleeding or bruising, black, tarry stools, blood in the urine or stools, or pinpoint red spots on your skin.
• Be careful when using a regular toothbrush, dental floss, or toothpick. Your medical doctor, dentist, or nurse may recommend other ways to clean your teeth and gums. Check with your medical doctor before having any dental work done.
• Do not touch your eyes or the inside of your nose unless you have just washed your hands and have not touched anything else in the meantime.
• Be careful not to cut yourself when you are using sharp objects such as a safety razor or fingernail or toenail cutters.
• Avoid contact sports or other situations where bruising or injury could occur.

Check with your doctor right away if you are rapidly gaining weight, having chest pain, extreme tiredness or weakness, irregular breathing, irregular heartbeat, or excessive swelling of the face, hands, wrist, ankles, or feet. These may be symptoms of fluid retention (too much water in your body).

Check with your doctor right away if you have stomach pain, pale stools or dark urine, loss of appetite, or yellow eyes or skin. These could be symptoms of a serious liver problem.

Check with your doctor right away if you have chest pain or tightness, decreased urine output, dilated neck veins, extreme fatigue, irregular breathing, irregular heartbeat, swelling of the face, fingers, feet, or lower legs, trouble breathing, weight gain. These could be symptoms of a serious heart problem.

This medicine may cause serious kidney problem. Check with your doctor right away if you have agitation, coma, confusion, decreased urine output, depression, dizziness, headache, hostility, irritability, lethargy, muscle twitching, nausea, rapid weight gain, seizures, stupor, swelling of the face, ankles, or hands, or unusual tiredness or weakness.

Cancer medicines can cause diarrhea, nausea, vomiting, or stomach pain, even after receiving medicines to prevent it. Ask your doctor or nurse about ways to control these side effects.

Talk with your doctor before using this medicine if you plan to have children. Some men and women using this medicine have become infertile (unable to have children).

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal (eg, St. John's wort) or vitamin supplements.

Side Effects of This Medicine:

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common

Black, tarry stools

bleeding gums

blood in the urine or stools

chest tightness

chills

cough

difficult or labored breathing

fever

lower back or side pain

painful or difficult urination

pale skin

pinpoint red spots on the skin

sore throat

swelling of the hands, ankles, feet, or lower legs

trouble breathing

ulcers, sores, or white spots in the mouth

unusual bleeding or bruising

unusual tiredness or weakness

Less common

Agitation

chest pain or discomfort

clay-colored stools

cough with mucus

confusion

dark urine

decreased appetite

decreased urination

depression

diarrhea

dizziness

dry mouth

fainting

fast or irregular heartbeat

general feeling of discomfort or illness

headache

hives, itching, or skin rash

hoarseness

hostility

increased sweating

increased thirst

irritation

joint pain, stiffness or swelling

lightheadedness

loss of appetite

muscle aches, pains, or twitching

nausea

numbness or tingling in the hands, feet, or lips

rapid breathing

rapid weight gain

redness of the skin

runny nose

seizures

shivering

sneezing

stomach pain or tenderness

sunken eyes

swelling of the eyelids, face, lips, hands, or feet

thirst

trouble sleeping

trouble swallowing

vomiting

weakness or heaviness of the legs

wrinkled skin

Rare

Blistering, peeling, or loosening of the skin

bloating

blue lips, fingernails, or skin

chest pain, possibly moving to the left arm, neck, or shoulder

constipation

coughing that sometimes produces a pink frothy sputum

difficult, noisy breathing

indigestion

irregular, fast or slow, or shallow breathing

pains in the stomach, side, or abdomen, possibly radiating to the back

puffiness or swelling of the eyelids or around the eyes, face, lips or tongue

red, irritated eyes

vomiting of blood or material that looks like coffee grounds

yellow eyes or skin

Incidence not known

Sudden, severe chest pain

sudden weakness in arms or legs

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

Back pain

difficulty with moving

lack or loss of strength

muscle stiffness

stuffy nose

Less common

Blemishes on the skin

burning feeling in the chest or stomach

change in taste

hearing loss

loss of taste

muscle cramping

pimples

ringing, buzzing, or other unexplained noise in the ears that continues

stomach upset

Rare

Flaking and falling off of the skin

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.